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Dietary polyphenols Rutin, Taxifolin and Quercetin related compounds target Leishmania amazonensis arginase

Abstract

Quercetin related compounds were tested against Leishmania amazonensis arginase, a potential target for the development of new approaches in treating leishmaniasis. The IC50 and kinetic analysis were performed to determine the dissociation constant Ki and the inhibition mechanism of the parasite's arginase enzyme. The best arginase inhibition was obtained from taxifolin (dihydroquercetin) with IC50 = 1.6 ± 0.1 µM. This study showed for the first time that rutin (IC50 = 10.4 ± 0.8 µM), and human metabolite quercetin-3-O-glucuronide (IC50 = 8.2 ± 0.4 µM), target L. amazonensis arginase. In addition, computational studies applying molecular docking simulations were performed to gain insight into the molecular basis for arginase inhibition by the competitive inhibitors. Our results suggest that these compounds could be exploited to develop new approaches for treating leishmaniasis through molecular nutrition supplement in a drug-based therapy.

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Publication details

The article was received on 08 Feb 2019, accepted on 15 May 2019 and first published on 16 May 2019


Article type: Paper
DOI: 10.1039/C9FO00265K
Food Funct., 2019, Accepted Manuscript

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    Dietary polyphenols Rutin, Taxifolin and Quercetin related compounds target Leishmania amazonensis arginase

    E. R. da Silva, S. Brogi, J. F. Lucon-Junior, G. Campiani, S. Gemma and C. C. Maquiaveli, Food Funct., 2019, Accepted Manuscript , DOI: 10.1039/C9FO00265K

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